Design and synthesis of tamoxifen derivatives as a selective estrogen receptor down-regulator

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• 作者：Takuji Shoda ; Keiichiro Okuhira ; Masashi Kato ; Yosuke Demizu ; Hideshi Inoue ; Mikihiko Naito ; Masaaki Kurihara
• 关键词：Breast cancer ; Estrogen receptor ; SERD ; Tamoxifen
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：1 January, 2014
• 年：2014
• 卷：24
• 期：1
• 页码：87-89
• 全文大小：519 K

文摘

We designed and synthesized an estrogen receptor (ER) down-regulator (5), which is a derivative of tamoxifen with a long alkyl side chain. Compound 5 effectively reduced ER protein levels in MCF-7 cells and had an antagonistic effect.